Medicine (MD/DO)
Lipid-lowering Agents
Atorvastatin (Lipitor)

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Atorvastatin (Lipitor)

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Atorvastatin (Lipitor)

Atorvastatin is an HMG-CoA reductase inhibitor and belongs to the statin class of medications. These medications end with the suffix “-statin” and are relatively similar. Statins inhibit the enzyme HMG-CoA reductase, which normally catalyzes the rate-limiting step in cholesterol biosynthesis. Inhibition of this enzyme results in reduction of levels of bad cholesterol (LDL) and triglycerides and increasing levels of good cholesterol (HDL). Statins are indicated in the treatment of hypercholesterolemia. Side effects can include rash, hepatotoxicity, and myopathy potentially leading to rhabdomyolysis. Therefore, it is recommended that liver enzymes be monitored at onset of therapy and repeated if signs of liver damage develop. HMG-CoA reductase inhibitors should be taken at bedtime and grapefruit juice should be avoided, as the latter can interfere with statin metabolism via the cytochrome P450 enzyme pathway.
-statin Suffix

Drugs in this class end with the “statin” suffix and generally have a similar mechanism of action and effect.

HMG-CoA Reductase Inhibitors
Hummingbird Coin-A-purse with Red-duck and Inhibiting-chains

Statins inhibit the enzyme HMG-CoA reductase, which normally catalyzes the rate-limiting step in cholesterol biosynthesis. HMG-CoA reductase inhibitors are effective at decreasing low-density lipoprotein (LDL) and total cholesterol levels. Further, this class may increase the “good cholesterol”, referred to as high-density lipoprotein (HDL) and decrease triglycerides. This mechanism has been found to decrease the risk of heart disease and sudden death.

High Cholesterol
High Cholesterol-burger

HMG-CoA reductase inhibitors are indicated for the treatment of high cholesterol levels (hypercholesterolemia). This class of medications decreases the “bad cholesterol” (low density lipoprotein, LDL) and triglycerides, while simultaneously increasing the “good cholesterol” (high density lipoprotein, HDL), although the effects on HDL are a little more variable.

Liver with Toxic-green-glow

Hepatotoxicity may occur in patients receiving statin medications. The liver is responsible for the production of cholesterol; therefore, these medications may cause injury to hepatocytes. If signs or symptoms of liver injury such as jaundice develop, liver function tests should be performed.


One of the side effects of statins is the development of a rash.


Rhabdomyolysis, or the breakdown of muscle cells, can occur with statin use. Statins can damage myocytes and lead to myopathy. If this persists, rhabdomyolysis can occur as damaged cells release myoglobin into the bloodstream. This myoglobin is filtered into the kidneys and broken down into heme pigment. Heme pigment is toxic to the kidneys and results in acute kidney injury (AKI). A mainstay of treatment is judicious IV hydration.


Myopathy, or injury to muscle tissue, may occur with use of high-dose statins. Patients receiving statin therapy should be monitored for diffuse or local muscle aches, weakness, and tenderness. Creatinine kinase (CK) levels in the serum can be checked to assess for muscle cell damage in myositis or the more severe problem of rhabdomyolysis.

Monitor Liver Enzymes
Monitor with Liver Enzymes

Because statins may cause liver damage, liver enzymes should be checked before starting this medication, and repeated if clinical concern for liver damage arises.

Administer at Bedtime
Eating in Bed

The liver produces the majority of cholesterol at night time. For this reason it is recommended that statins are administered at bedtime.

Avoid Grapefruit
Avoid-sign Grapefruit

Grapefruits and their juice should be avoided in patients taking statins because grapefruits contain chemicals that inhibit the enzyme CYP3A4, causing levels of the statin to rise.


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